research use only
Cat.No.S1778
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase |
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| Other Thymidylate Synthase Inhibitors | Raltitrexed |
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In vitro |
DMSO
: 59 mg/mL
(199.18 mM)
Water : 59 mg/mL Ethanol : 59 mg/mL |
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In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 296.2 | Formula | C10H11F3N2O5 |
Storage (From the date of receipt) | |
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| CAS No. | 70-00-8 | Download SDF | Storage of Stock Solutions |
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| Synonyms | NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT | SMILES | C1C(C(OC1N2C=C(C(=O)NC2=O)C(F)(F)F)CO)O | ||
Read more about storage stability stock solution CAS number SMILES
| Targets/IC50/Ki |
DNA synthesis
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| In vitro |
Trifluridine (NSC 75520) inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently. It also inhibits colony formation of bone marrow cells in a concentration-dependent manner. This compound and 2'-deoxy-5-fluorouridine (FdUrd) are incorporated into DNA with different efficiencies due to differences in the substrate specificities of TK1 and DUT, causing abundant FTD incorporation into DNA. FTD-treated cells shows differing nuclear morphologies compared to FdUrd-treated cells. It further inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently.
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| In vivo |
Trifluridine (NSC 75520) has significantly fewer swabs positive for HSV-1 than the untreated eyes in the infected rabbits. This compound has increased antitumor activity and is incorporated into DNA more effectively than continuously infused Trifluridine in mice. It gradually accumulates in tumor cell DNA, in a TPI-independent manner, and significantly delays tumor growth and prolonged survival in mice, compared to treatment with 5-FU derivatives. Furthermore, it results in significantly lower viral titers, fewer HSV-1-positive eyes/total during the treatment period, lower keratitis scores, fewer eyes with keratitis/total, and a shorter time to resolution of keratitis in the New Zealand rabbit ocular model.
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References |
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(data from https://clinicaltrials.gov, updated on 2026-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06197425 | RECRUITING | Colon or Upper Rectum Adenocarcinoma |
Centre Hospitalier Universitaire Dijon |
2026-05-07 | PHASE3 |
| NCT07381764 | NOT_YET_RECRUITING | Metastatic Colorectal Cancer (CRC) |
Gruppo Oncologico Italia Meridionale |
2026-03-30 | PHASE2 |
| NCT07270991 | RECRUITING | Metastatic Oesogastric Adenocarcinoma |
Federation Francophone de Cancerologie Digestive |
2025-12-15 | PHASE3 |
| NCT05719558 | RECRUITING | Advanced Solid Tumors |
Astellas Pharma Global Development, Inc. |
2023-03-13 | PHASE1 |
| NCT06856837 | RECRUITING | Metastatic Colorectal Cancer |
Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest |
2025-10-27 | PHASE2 |
| NCT07286695 | NOT_YET_RECRUITING | Metastatic Colorectal Cancer (CRC); Colorectal Cancer |
Cancer Institute and Hospital, Chinese Academy of Medical Sciences |
2025-12-31 | PHASE2 |
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